A kind of preparation method of Axitinib tablet

Abstract

The invention provides a method for preparing axitinib tablets through a dry powder tabletting method.The method comprises the steps that 1, raw and auxiliary material components comprising 0.5 wt%-3 wt% of axitinib, 85 wt%-97 wt%of a diluent, 1 wt%-10 wt% of a disintegrating agent and 0.25 wt%-2 wt% of a lubricating agent are weighed; 2, the axitinib and the auxiliary materials are mixed in batches; 3, a mixture obtained in the step 2 is tabletted and coated to obtain the axitinib tablets, wherein the particle size D90 of the axitinib is smaller than or equal to 60 micrometers, the particle size of at least 90% of the diluent is smaller than 240 micrometers, the particle size of at least 30% of the diluent ranges from 50 micrometers to 140 micrometers, and the particle size of 2-20 wt% of the diluent is smaller than 32 micrometers.The method for preparing the axitinib tablets through the dry powder tabletting method is simple and reliable; the axitinib tablets prepared through the method are uniform in content, small in tablet weight difference, low in tablet cracking rate and qualified in dissolution curve, and the related substance content meets the specification; meanwhile, the method has the advantages that the technology is simple, the production period is short, the production efficiency is improved, and the cost is reduced.

Description

technical field [0001] The invention relates to a preparation method of axitinib tablet. Background technique [0002] Axitinib (Axitinib) is a multi-target tyrosine kinase inhibitor developed by Pfizer, which can inhibit vascular endothelial cell growth factor receptors VEGFR1, VEGFR2, VEGFR3, platelet-derived growth factor receptor and c-KIT. It was approved for marketing by the FDA on January 27, 2012, for advanced renal cancer ineffective to other systemic treatments. The currently marketed axitinib products are tablets. [0003] Tablet is one of the most widely used dosage forms of pharmaceutical preparations at present. Its preparation methods can be divided into two categories: granulation and tableting method and whole powder tableting method. and dry granulation tableting. [0004] Axitinib itself is unstable to light and is prone to degradation in the presence of heat or water, resulting in the increase of related substances in the preparation. However, the pre...

AI Technical Summary

Problems solved by technology

But at the same time, the smaller the particle size of axitinib, the harder it is to mix evenly

From the perspective of excipients, since the materials for all-powder tableting are in the form of powders, the fluidity and compressibility of excipients are high, so it is difficult to choose the appropriate type and proportion of excipients.

In addition, the particle size distribution of excipients is crucial to the quality of the tablet. If the particle size of the excipient is too large, it is easy to mix unevenly with axitinib; while the particle size of the excipient is too small, the fluidity of the material will be poor. , poor compressibility, easy to cause splits, even can not be pressed into tablets

[0010] It can be seen that the difficulty of preparing Axitinib tablets by the full powder compression method is relatively large, and the inventor believes that this is an important reason why no one adopts the full powder compression method to prepare Axitinib tablets in the prior art.

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